Synthesis, characterization, and antitumor activity of some novel S-functionalized benzo[d]thiazole-2-thiol derivatives; regioselective coupling to the –SH group

2018 ◽  
Vol 73 (9) ◽  
pp. 647-654
Author(s):  
El Sayed Ramadan ◽  
Hamida M. Abdel Hamid ◽  
Sawsan A. Noureddin ◽  
Khadija O. Badahdah
Keyword(s):  
Antitumor Activity ◽  
Sodium Hydride ◽  
Ultrasound Irradiation ◽  
Ehrlich Ascites Carcinoma ◽  
Antitumor Antibiotic ◽  
Ehrlich Ascites ◽  
Quinoxaline Derivatives ◽  
Sh Group ◽  
Eac Cells

AbstractSeveral 2-substituted sulfanyl benzo[d]thiazoles were regioselectively synthesized by the reaction of benzo[d]thiazole-2-thiol (1a) with a variety of reagents under different basic conditions. Some 2-(2,3-disubstituted propyl sulfanyl)benzo[d]thiazoles were obtained from 2-(allylthio)benzo[d]thiazole, which was prepared by the allylation of 1a with allyl bromide in the presence of sodium hydride in dry N,N-dimethylformamide. Reaction of 1a with various pyrazolyl-quinoxaline derivatives was also investigated. Better yields and shorter reaction time were achieved for the synthesis of some derivatives by using ultrasound irradiation. The structural elucidation of all compounds was based on both analytical and spectroscopic data. The newly synthesized compounds were tested in vitro for their antitumor activity against Ehrlich ascites carcinoma (EAC) cells grown in albino mice. Doxorubicin was used as a standard antitumor antibiotic, and some compounds showed half maximal inhibitory concentration (IC50) in the range 40–68 μg mL−1.

Evaluation of Cisplatin Combined with Ondansetron in Ehrlich Ascites Carcinoma in Vitro and in Vivo

2000 ◽  
Vol 86 (2) ◽  
pp. 153-156 ◽  
Author(s):  
Osama Ahmed Badary ◽  
Sahar Moustafa Sharaby ◽  
Sanaa Abd El-Baky Kenawy ◽  
Ezz El-Deen El-Denshary ◽  
Farid Mohamed Ahmed Hamada
Keyword(s):  
Antitumor Activity ◽  
Ehrlich Ascites Carcinoma ◽  
Host Tissue ◽  
Nausea And Vomiting ◽  
Single Treatment ◽  
Blood Cell Count ◽  
Ehrlich Ascites ◽  
Eac Cells

Aims and background Nausea and vomiting occur in the majority of patients receiving cisplatin (CDDP) chemotherapy. Ondansetron, a new 5-HT3 receptor antagonist, has been used effectively to control CDDP-induced nausea and vomiting. This study examined the potential of ondansetron to interfere with CDDP antitumor activity and toxicity in Ehrlich ascites carcinoma (EAC). Methods The influence of ondansetron on CDDP cytotoxicity was evaluated using EAC cells in culture. In addition, the influence of ondansetron pretreatment on CDDP-induced antitumor activity and host tissue toxicity was studied in EAC-bearing mice. Results Ondansetron (0.25 μM) enhanced CDDP (0–32 μM) cytotoxicity against EAC cells in vitro. In EAC-bearing mice ondansetron (0.2 mg/kg, ip) administered 1 h before CDDP (7 mg/kg, ip) did not modify the antitumor activity of CDDP. CDDP (7 mg/kg, ip) single treatment induced significant increases in blood urea nitrogen (2-fold) and serum creatinine (2.5-fold) and significant decreases in hematocrit (25%) and white blood cell count (39%) compared to saline treatment. Mice receiving ondansetron 1 h before CDDP showed no significant enhancement of CDDP-induced nephrotoxicity or myelosuppression compared to those pretreated with saline receiving the same dose of CDDP. Conclusions This study suggests that the use of ondansetron to control CDDP-induced nausea and vomiting does not affect CDDP antitumor efficacy.

Tumor cell metabolism in vitro: a study of incubation media

1970 ◽  
Vol 48 (4) ◽  
pp. 517-519 ◽  
Author(s):  
I. C. Caldwell ◽  
Marianne F. Chan
Keyword(s):  
Nucleic Acid ◽  
Structural Integrity ◽  
Cell Metabolism ◽  
Ehrlich Ascites Carcinoma ◽  
Leukemic Cells ◽  
Prolonged Incubation ◽  
Ehrlich Ascites ◽  
Eac Cells ◽  
Rna And Dna

A number of incubation media which have been used in studies of the metabolism of Ehrlich ascites carcinoma (EAC) cells in vitro have been examined with respect to their abilities to support the incorporation of radioactive precursors into nucleotides and nucleic acids, and to maintain the structural integrity and tumor-inducing abilities of EAC cells. Cells incubated in the chemically-defined "Fischer's medium for leukemic cells of mice" were able to produce lethal tumors in mice after more than 16 h of incubation, maintained their structural integrity on prolonged incubation, and catalyzed high rates of incorporation of exogenously added substrates into nucleotides, RNA, and DNA. However, cells incubated in balanced salts solutions supplemented with glucose had these characteristics: (a) were unable to produce lethal tumors after 4 h of incubation, (b) released large amounts of nucleotide, nucleic acid, and protein material into the medium after less than 2 h of incubation, and (c) catalyzed the incorporation of radioactive precursors into nucleotides and RNA at much lower rates than did cells incubated in Fischer's medium, and were virtually unable to catalyze the incorporation of adenine-14C into DNA.

scholarly journals In vitro and in vivo evaluation of antitumor activity of methanolic extract of Argyreia nervosa leaves on Ehrlich ascites carcinoma

2015 ◽  
Vol 10 (2) ◽  
pp. 399
Author(s):  
Bhawna Sharma ◽  
Isha Dhamija ◽  
Sandeep Kumar ◽  
Hema Chaudhary
Keyword(s):  
Antitumor Activity ◽  
Solid Tumor ◽  
Methanolic Extract ◽  
Ehrlich Ascites Carcinoma ◽  
Ehrlich Ascites ◽  
Wide Range ◽  
Antioxidant Parameters ◽  
Argyreia Nervosa

<p>The herb of importance like <em>Argyreia nervosa</em> has shown wide range of pharmacological activities. Its methanolic extract of <em>A. nervosa</em> has been explored against Ehrlich ascites carcinoma (EAC) induced liquid and solid tumor in mice. Liquid and solid tumors were induced by intraperitoneal and subcutaneous transplantation of EAC cells in Balb/C mice. Significant and dose dependant results are observed when the mice are sacrificed on 15<sup>th</sup> day for estimation of tumor proliferation, hematological, biochemical and hepatic antioxidant parameters. Mean survival time (days) was increased to 36.5 from 20.5 extract treated mice. The extract also showed a decrease (p&lt;0.001) in body weight and percentage reduction in tumor volume respectively when it was evaluated in solid tumor induced mice for a period of 30 days.  From the result it was concluded that the extract has as a potent antitumor activity and that is comparable to 5-fluorouracil.</p><p> </p>

scholarly journals In vivo Anticancer Activity on Ehrlich Ascites Carcinoma (EAC) Cells and in vitro Antimicrobial Activity of Psidium guajava Bark Extracts

2019 ◽  
Vol 35 (1) ◽  
pp. 79-81
Author(s):  
Md Jakir Hossain ◽  
Shashwata Biswas ◽  
Mohammad Shahriar ◽  
Sohidul Islam ◽  
Chowdhury Rafiqul Ahsan
Keyword(s):  
Antimicrobial Activity ◽  
Anticancer Activity ◽  
Methanol Extract ◽  
Ehrlich Ascites Carcinoma ◽  
Psidium Guajava ◽  
Negative Control ◽  
Ehrlich Ascites ◽  
Eac Cells

This study was performed to evaluate the in vivo anticancer activity against ehrlich ascites carcinoma (EAC) cells and in vitro antimicrobial activity of Psidium guajava bark extracts. By soxhlet apparatus, the P. guajava bark extracts were obtained using four solvents (n-hexane, petroleum benzene, chloroform, and methanol) according to their increasing solubility. In case of in vivo anticancer activity of the sample extracts, mice were seeded with approximately 1x105 ehrlich ascites carcinoma (EAC) cells. After seven days of consecutive treatment, the negative and positive control groups (n=8 each group) showed an average EAC cell count of 2.4x108 and 1.8x108 respectively, and the experimental groups showed the cell count of 2.2x 108, 2.1x108, 1.9x108, and 1.41x108 when mice received h-hexane, petroleum benzene, chloroform, and methanol extract respectively. Experimental group that received methanol extract showed percent increase of life span (% ILS) of 33.3 when compared with the negative control. However, treatment in a cyclic manner of the mice showed % ILS of 52.15 for experimental group when compared negative control. In antimicrobial activity experiment, an intermediate zone of sensitivity of the crude methanol extract was found against Escherichia coli, Shigella flexneri, and Staphylococcus aureus when compared with amoxicillin. All these results indicated the anticancer activity and antimicrobial activity of the methanol extract of P. guajava barks on different experimental models. Bangladesh J Microbiol, Volume 35 Number 1 June 2018, pp 79-81

2', 4'-dihydroxy-3, 4-methylenedioxychalcone Activate Mitochondrial Apoptosis of Ehrlich Ascites Carcinoma Cells

2020 ◽  
Vol 15 (4) ◽  
pp. 337-350
Author(s):  
Mahbuba Khatun ◽  
Farhadul Islam ◽  
Vinod Gopalan ◽  
Md. Motiar Rahman ◽  
Natasha Zuberi ◽  
...  
Keyword(s):  
Growth Inhibition ◽  
Chromatin Condensation ◽  
In Vitro Study ◽  
Ehrlich Ascites Carcinoma ◽  
Dependent Manner ◽  
Anticancer Properties ◽  
Ehrlich Ascites ◽  
Induced Apoptosis ◽  
Eac Cells

Background: Development of effective cancer-chemotherapy is the most challenging field due to the toxicity of chemo-agents. Objective: As chalcone has been known to have pharmacological applications, here the aim is to synthesized three chalcone derivatives, 2',4'-dihydroxy-3,4-methylenedioxychalcone (C1), 2'-hydroxy- 2,4, 6-trimethoxychalcone (C2) and 2'-hydroxy-4-methylchalcone (C3) and investigate their anti-cancer properties against Ehrlich Ascites Carcinoma (EAC) cell. Method: Anticancer properties against EAC cells were studied by examining growth inhibition, MTT assays, tumour-bearing mice survival, tumour weight measurement and haematological profiles. Moreover, apoptosis of EAC cells was investigated by fluorescence microscopy, flowcytometry and DNA fragmentation assays. Expression of apoptosis related genes were studied by reverse transcriptase-PCR (RT-PCR). Results: Among the compounds, C1 exhibited highest cell growth inhibition at 200 mg/kg/day (81.71%; P < 0.01). C1 treatment also increased the life span of EAC-bearing mice (82.60%, P < 0.05) with the reduction of tumour burden (22.2%, P < 0.01) compared to untreated EAC-bearing mice. In vitro study indicated that C1 killed EAC-cells in a dose-dependent manner and induced mitochondria-mediated apoptotic pathways. In addition, C1 treated cells exhibited increased apoptotic features such as membrane blebbing, chromatin condensation, and nuclear fragmentation after Hoechst 33342 staining. Increased fragmentation of DNA in gel electrophoresis followed by C1 treatment further confirmed apoptosis of EAC cells. EAC cells treated with C1 showed reduced Bcl-2 expression in contrast to notable upregulation of p53 and Bax expression. It implied that C1 could reinstate the expression of pro-apoptotic tumour suppressor and inhibit anti-apoptotic genes. Conclusions:: Thus, C1 showed significant growth inhibitory properties and induced apoptosis of EAC cells.

scholarly journals Antineoplastic Activities of MT81 and Its Structural Analogue in Ehrlich Ascites Carcinoma-Bearing Swiss Albino Mice

2010 ◽  
Vol 3 (1) ◽  
pp. 61-70 ◽  
Author(s):  
Sujata Maiti Choudhury ◽  
Malaya Gupta ◽  
Upal Kanti Majumder
Keyword(s):  
Cell Count ◽  
Tumor Volume ◽  
Ehrlich Ascites Carcinoma ◽  
Viable Tumor Cell ◽  
Structural Analogue ◽  
Mean Survival Time ◽  
Ehrlich Ascites ◽  
Eac Cells

Many fungal toxins exhibit in vitro and in vivo antineoplastic effects on various cancer cell types. Luteoskyrin, a hydroxyanthraquinone has been proved to be a potent inhibitor against Ehrlich ascites tumor cells. The comparative antitumor activity and antioxidant status of MT81 and its structural analogue [Acetic acid-MT81 (Aa-MT81)] having polyhydroxyanthraquinone structure were assessed against Ehrlich ascites carcinoma (EAC ) tumor in mice. The in vitro cytotoxicity was measured by the viability of EAC cells after direct treatment of the said compounds. In in vivo study, MT81 and its structural analogue were administered (i.p.) at the two different doses (5, 7 mg MT81; 8.93, 11.48 mg Aa-MT81/kg body weight) for 7 days after 24 hrs. of tumor inoculation. The activities were assessed using mean survival time (MST), increased life span (ILS), tumor volume, viable tumor cell count, peritoneal cell count, protein percentage and hematological parameters. Antioxidant status was determined by malondialdehyde (MDA) and reduced glutathione (GSH ) content, and by the activity of superoxide dismutase (SOD) and catalase (CA T). MT81 and its structural analogues increased the mean survival time, normal peritoneal cell count. They decreased the tumor volume, viable tumor cell count, hemoglobin percentage and packed cell volume. Differential counts of WBC, total counts of RBC & WBC that altered by EAC inoculation, were restored in a dose-dependent manner. Increased MDA and decreased GSH content and reduced activity of SOD, and catalase in EAC bearing mice were returned towards normal after the treatment of MT81 and its structural analogue. Being less toxic than parent toxin MT81, the structural analogue showed more prominent antineoplastic activities against EAC cells compared to MT81. At the same time, both compounds exhibit to some extent antioxidant potential for the EAC-bearing mice.

scholarly journals MytiLec-1 Shows Glycan-Dependent Toxicity against Brine Shrimp Artemia and Induces Apoptotic Death of Ehrlich Ascites Carcinoma Cells In Vivo

Marine Drugs ◽  
2019 ◽  
Vol 17 (9) ◽  
pp. 502 ◽  
Author(s):  
Imtiaj Hasan ◽  
A.K.M. Asaduzzaman ◽  
Rubaiya Rafique Swarna ◽  
Yuki Fujii ◽  
Yasuhiro Ozeki ◽  
...  
Keyword(s):  
Cell Growth ◽  
Ehrlich Ascites Carcinoma ◽  
Cancer Cell Growth ◽  
Artemia Nauplii ◽  
Ehrlich Ascites ◽  
Diphenyltetrazolium Bromide ◽  
Mediterranean Mussel ◽  
Eac Cells

MytiLec-1, a 17 kDa lectin with β-trefoil folding that was isolated from the Mediterranean mussel (Mytilus galloprovincialis) bound to the disaccharide melibiose, Galα(1,6) Glc, and the trisaccharide globotriose, Galα(1,4) Galβ(1,4) Glc. Toxicity of the lectin was found to be low with an LC50 value of 384.53 μg/mL, determined using the Artemia nauplii lethality assay. A fluorescence assay was carried out to evaluate the glycan-dependent binding of MytiLec-1 to Artemia nauplii. The lectin strongly agglutinated Ehrlich ascites carcinoma (EAC) cells cultured in vivo in Swiss albino mice. When injected intraperitoneally to the mice at doses of 1.0 mg/kg/day and 2.0 mg/kg/day for five consecutive days, MytiLec-1 inhibited 27.62% and 48.57% of cancer cell growth, respectively. Antiproliferative activity of the lectin against U937 and HeLa cells was studied by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay in vitro in RPMI-1640 medium. MytiLec-1 internalized into U937 cells and 50 μg/mL of the lectin inhibited their growth of to 62.70% whereas 53.59% cell growth inhibition was observed against EAC cells when incubated for 24 h. Cell morphological study and expression of apoptosis-related genes (p53, Bax, Bcl-X, and NF-κB) showed that the lectin possibly triggered apoptosis in these cells.

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